Abstract: The syn isomer of (R) or (S) or (R,S) mixture, in the form of internal salts or salts with acids or bases of a compound of the formula ##STR1## wherein the substituents are defined as in the specification having a very good antibiotic activity.

Abstract: The invention provides a pyrazolo?1,5-a!pyrimidine derivative of the following formula (1): ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.6, Q, A and n are defined in the description; and R.sup.2 is naphthyl, cycloalkyl, furyl, thienyl, optionally halogen-substituted pyridyl, optionally halogen-substituted phenoxy, or phenyl which may have 1 to 3 substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro, halogen-substituted lower alkyl, halogen-substituted lower alkoxy, lower alkoxycarbonyl, hydroxyl, phenyl(lower)alkoxy, amino, cyano, lower alkanoyloxy, phenyl and di(lower)alkoxyphos-phoryl(lower)alkyl. This derivative is useful as a potent analgesic.

Abstract: Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.

Abstract: The present invention relates to a nitrogen-containing heterocyclic compound exhibiting an inhibitory activity against cGMP-PDE. The compound represented by the formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a group represented by the formula: --NR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 each represent hydrogen, lower alkyl or the like) or the like; R.sup.2 represents a group represented by the formula: ##STR2## (wherein R.sup.8 represents a carboxyl group which may be protected, or the like) or the like; and R.sup.3 represents a group represented by the formula: ##STR3## (wherein R.sup.6 and R.sup.7 each represent hydrogen, lower alkyl or the like) or the like.

Abstract: A compound of the formula: ##STR1## or its salt is prepared by reacting a compound of the formula: ##STR2## with a compound of the formula: ##STR3## Wherein the variables are all defined in claim 1.

Abstract: Herbicidal 4-cycloalkyl-5-substituted pyrimidine compounds of the formula ##STR1## are described. Herbicidal compositions containing such substituted-pyrimidinyl compounds and methods of controlling undesirable vegetation employing these compounds are also disclosed. The compounds in which XR, is hydroxyl are also useful as intermediates for producing the disclosed substituted-pyrimidinyl derivatives.

Abstract: The present invention relates to pyrimido?5,4-d!pyrimidines of the general formula ##STR1## in which R.sub.a to R.sub.c are as defined herein, their tautomers, their stereoisomers and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibiting action on signal transduction mediated by tyrosine kinases, their use for the treatment of diseases, in particular tumor diseases.

Abstract: Novel process for preparing azetidinone compound of the formula ?III!: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula ?I!: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula ?II!: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound ?Ill! being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.

Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.

Abstract: Compounds of formula I ##STR1## wherein X.sup.a, X.sup.b, R, R.sup.1 and R.sup.2 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful as potassium channel openers for the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The present invention provides a process for producing an N-vinyl compound, which comprises subjecting an N-(-alkoxyalkyl) compound to gas phase intramolecular alcohol elimination to convert said compound to an N-vinyl compound directly in one step, wherein a solid oxide containing phosphorus and an alkali metal and/or an alkaline earth metal is used as a catalyst. This process need not use any solvent or any auxiliary raw material and consequently can produce an N-vinyl compound simply and safely without generating any waste material derived from the auxiliary raw material.

Abstract: A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two hydroxy moieties, an ether or ester thereof (e.g., a polyether ester, heterocyclic ester amino acid ester or phosphate ester) thereof and the carbon with the asterisk (*) has the R or S absolute configuration or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

Abstract: The invention relates to crop protection agents which comprise an active substance combination of herbicide and safener. The herbicides are selected from the group comprising the ALS inhibitors (ALS=acetolactate synthase) such as sulfonylureas, imidazolines, triazolopyrimidinesulfonamides, pyrimidyloxypyridinecarboxylic acid derivatives and pyrimidyloxybenzoic acid derivatives. The safeners are compounds of the formula I ##STR1## which are as defined in claim 1, where Z and Y are N or CH, it being possible for H to be replaced by X,X is H, Hal, haloalkyl or -alkoxy, alkyl, alkoxy, alkylthio, NO.sub.2, NH.sub.2, CN, alkylsulfonyl,A is alkylene or alkenylene,B is carboxyl or a derivative of the carboxyl group.The mixtures are mainly suitable for controlling harmful plants in the crops maize and cereals.

Abstract: Novel 1,3-oxazin-4-one derivatives of the formula ##STR1## wherein R.sup.1 to R.sup.5 are hydrocarbyl radicals which are optionally substituted, and herbicidal compositions comprising the same as active ingredients and their use in controlling the growth of weeds. The compounds can be produced by reacting substituted 1,3-dioxin-4-one derivatives and N-methylene-alkylamine.

Abstract: Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.

Abstract: This invention is directed to bicyclic pyrimidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: Polymorphic forms of the angiotensin II receptor antagonist, 3-?2'-(N-benzoyl)sulfonamidobiphenyl-4-yl!methyl-5,7-dimethyl-2-ethyl-3H-i midazo?4,5-b!pyridine and a method for the preparation of these crystal forms.

Abstract: Nitrobenzyl mustard quaternary salts of formula (I), ##STR1## and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR.sub.1 R.sub.2 -- or CR.sub.1 .dbd.CR.sub.2-- (where R.sub.1 and R.sub.2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO.sub.2 R; Q is lower alkyl (optionaly substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or other groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO.sub.2, SO.sub.2 R, CONHR, R, OR, SR, CF.sub.3 and aza (ring --CH.dbd.replaced by --N.dbd.); with the proviso that when H-Cl or Br, Q=Me, and X=CH.sub.2 -- then Ar.noteq.2-nitrophenyl or 4-nitrophenyl.

Abstract: Novel O.sup.6 -substituted guanine compounds and pharmaceutical compositions thereof are useful for effectively reducing O.sup.6 -alkylguanine-DNA alkyltransferase (AGT). The novel compounds are useful for treating tumors and when used with anti-neoplastic alkylating agents enhance the chemotherapeutic treatment of tumor cells in a host.